Androgen receptorantagonist 1 is an orally available full androgen receptorantagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.
CXCR2 antagonist 4 (compound 7) is a highly potent antagonist that inhibits CXCR2 with an IC50 value of 0.13 μM. It also effectively inhibits the cytosolic calcium increase induced by CXCL8, with an IC50 value of 27 μM. CXCR2 antagonist 4 shows promising potential for anticancer research [1].
MrgprX2 antagonist-4 and compound B-51 E117, is a potent MrgprX2 antagonist. It specifically targets and inhibits the MrgprX2 receptor, making it suitable for investigating various inflammatory skin disorders.
NMDA receptorantagonist 2 is a highly potent and orally active NR2B subtype-selective antagonist of the N-methyl-D-aspartate (NMDA) receptor. It exhibits remarkable binding affinities, with an IC50 of 1.0 nM and a Ki value of 0.88 nM. This compound finds valuable application in scientific investigations focusing on neuropathic pain and Parkinson’s disease.
Substance P ReceptorAntagonist 1 has the potential function in gastrointestinal disorders, inflammatory diseases, respiratory, and central nervous system disorders.